Dermazol

Dermazol is a local, as well as a systemic antimycotic drug. It is a derivative of the substances triazole, as well as imidazole.

Indications of the dermazol

Tablets are used for systemic treatment of infectious pathologies of fungal origin, which have different localization, and are caused by microbes that are sensitive to the effect of ketoconazole. Among them:

• infection of the candida type on the mucous in the area of the intestine;
• prevention of the development of relapses or their treatment in patients with chronic stage of thrush;
• therapy for systemic mycoses (among them the systemic form of candidiasis, histoplasmosis with paracoccidomycosis and blastomycosis);
• elimination of diseases of fungal etiology in the area of skin and hair with nails (among them candidal onychia, trichophytosis, mycosis of nails, multicolored form of lichen, and in addition folliculitis, having a fungal genesis), in situations when local treatment did not work;
• also tablets are used to prevent the appearance of fungal pathologies in people with immunodeficiency.

Use of the cream - for local treatment with epidermophytosis in the limbs, as well as the groin, and with it with trichophytosis. In addition, the cream can be used to eliminate the following diseases:

• multi-colored form of lichen;
• Candidiasis in the area of the skin;
• seborrhea;
• Folliculitis, provoked by the bacterium Pityrosporum.

Shampoo Dermazol is prescribed in such cases:

• deprive a multicolored or otrubrious type in the area of the skin on the head;
• seborrheic form of dermatitis or eczema of seborrheic type on the scalp.

Release form

Release in the form of cream, tablets and shampoo.

Cream - in tubes with a volume of 15 or 30 g. Inside a single pack - 1 tube of medicine.

Tablets are available in 10 pieces inside the blister plate. In a separate package - 1-2 blisters with tablets.

Shampoo can be produced in flacons with a volume of 50 or 100 ml (1 bottle inside the pack), or in the form of a sachet (8 ml volume), 20 pieces inside the package.

Pharmacodynamics

The ketoconazole component is an artificial derivative of the imidazolidioxolane compound. It has antimycotic properties, acting against yeast with dermatophytes.

Ketoconazole has fungistatic, as well as fungicidal properties with respect to eumycetes with dermatophytes, and in addition fungi yeast or dimorphic type. In addition, the antimicrobial activity of the substance is also observed with respect to most strains of staphylococci with streptococci.

Penetrating into the fungal cell, the drug begins to suppress the synthesis of components that are the basis of the membrane of fungal cells. Thus, the biosynthesis of phospholipids with triglycerides, as well as ergosterol, is disrupted. Because of the decrease in the number of these elements inside the fungal cell, as well as the membrane itself, the structure of the cell membrane irreversibly changes. Fungistatic effect of the substance provides a reduction in the ability of the fungus to form colonies. Due to its fungicidal properties, the drug promotes a change in the structure of the membrane of fungal cells, as well as the weakening of its strength. As a result, the perforation of the membrane occurs, causing the fungus to die.

Dermazol is effective in eliminating fungi caused by bacteria such as Pityrosporum orbiculare, Candida fungi, cryptococci, flaky epidermophyton, Trichophyton spp., And Microsporum spp., And in addition to infections caused by Gram-positive cocci (including Streptococcus and Staphylococci ).

The substance ketoconazole has a strong fungicidal effect on the bacterium Pityrosporum ovate (it is because of it that dandruff appears).

After prolonged systemic use, the active component of the drug provokes a decrease in the processes of the biosynthesis of testosterone, as well as other androgenic hormones.

Pharmacokinetics

After taking the pill inside, the medicine is well absorbed inside the intestine. The absorption efficiency increases when there is an acidic environment. After oral administration, ketoconazole demonstrates high bioavailability (approximately 75%).

The medicine in high concentrations is observed inside the plasma, as well as tissues and other biological fluids. The highest rates are noted inside the kidneys with the liver, and in addition to the heart muscle and lungs. The substance is able to pass through the BBB, but its values inside the cerebral tissues are higher than the level inside the CSF. The effectiveness of the drug depends on the size of the dosage.

The peak plasma level of the active drug component is observed 1-2 hours after taking the tablet. Ketoconazole has a high degree of synthesis with a plasma protein (mainly - albumin).

Excretion from the plasma occurs in 2 phases. At the 1st half-life is 2 hours, and at the terminal - 8 hours.

The substance is metabolized, resulting in the formation of inactive decay products. Excretion of the drug is mainly carried out with bile, and about 15% is excreted in urine. Excretion of drugs occurs both in unchanged form and in the form of inactive decay products.

Dosing and administration

Tablets.

Dermazol tablets are taken orally, along with food, washed down with water.

For children weighing more than 30 kg, as well as adults during the treatment of systemic infections of the fungal type, the dosage is 200 mg (1 tablet) once a day. In case of severe course of the disease or if after some time of drug use in the patient no improvement is observed, it is allowed to increase the dose to 400 mg (2 tablets) - once a day.

The duration of the therapeutic course is prescribed by the treating doctor, taking into account the nature of the pathology, as well as the features of the condition and organism of the patient. Take the pill after the disappearance of all signs of the disease, as well as receiving a negative result of the mycological test should be at least 1-week.

To eliminate dermatological infections of the fungus type, provoked by dermatophytes, you should take the medicine in the period of 2-6 weeks.

When treating varicolored lichen, the duration of the course is basically 10 days.

When infections on the mucous membranes of the mouth and skin (Candida type), the course usually lasts within 2-3 weeks.

During the treatment of hair loss (fungal etiology), the drug should last at least 3 weeks / maximum 2 months.

With mycosis of the nails, the course often continues in the period of 0.5-1 (the more accurate figure depends on the speed with which the nails grow). You can stop the course only after the nail area has completely recovered from the disease.

During mycoids of the systemic type, the course generally lasts 1-6 months.

When treating or preventing the development of relapses during a chronic type of thrush, take 2 tablets once a day for a period of 5 days.

To prevent the emergence of fungal infections in people with immunodeficiency - children weighing more than 30 kg and adults are required to take 2 tablets of drugs once a day. Children weighing less than 30 kg should take the drug at a rate of 4-8 mg / kg per day.

Tablets are recommended to be consumed at the same time of day to maintain a stable level of drug concentration inside the plasma. If you miss the time of taking the pill, you should take it as soon as possible, but if you take less than 4 hours before the next dose, the missed pill should not be drunk.

Cream.

Cream should be treated affected areas 1-2 times per day.

The duration of therapy depends on the course of the pathology, but if no improvement is observed in the period of 4 weeks from the start of the drug use, it is required to clarify the correctness of the diagnosis.

During treatment of varicolored lichen or dermatological infections of the candida type, the course often lasts 2-3 weeks.

When eliminating cutaneous fungi, treatment generally lasts 3-4 weeks.

During elimination of the seborrheic form of dermatitis, the medication is usually applied in the period of 2-4 weeks.

Before and after the procedure, you should thoroughly wash your hands.

Shampoo.

The medicine in the form of a shampoo should be applied to washed damp hair, after which it should be foamed and held for several minutes, and then completely rinsed.

In multi-colored deprivation, shampoo should be applied to the hair once a day during a period of 5 days.

With the seborrheic form of dermatitis, the drug is also used once a day, but in the period of 3 days.

To prevent the appearance of dandruff or for its treatment, Dermazol should be used once a day at intervals of 7-14 days.

Use of the dermazol during pregnancy

Pregnant or lactating women can use the medicine in the form of shampoo or cream without restrictions, because ketoconazole in these dosage forms is not absorbed into the circulatory system and has no general effect.

But Dermazol in the form of tablets in this period is completely banned. If it is necessary to take drugs with lactation, you need to refuse for the period of treatment from breastfeeding - because ketoconazole penetrates into the mother's milk.

Contraindications

Contraindication for each form of the drug is intolerance with respect to ketoconazole.

Tablets can not be taken to people suffering from hepatic pathologies.

It is also forbidden to prescribe Dermazol in patients with porphyria.

Caution is required when used in people with adrenal insufficiency.

There is no information on the use of medicines in children.

Side effects of the dermazol

Due to systemic use of drugs, the development of such adverse reactions has been observed:

• reactions from the gastrointestinal tract and hepatobiliary system: vomiting, stool disorders, epigastric pains and nausea. Hepatitis can also develop and the activity of liver enzymes increase;
• manifestations of the central nervous system: dizziness and headaches, as well as photophobia;
• violations in the work of SSS and hematopoietic system: an increase in ICP, as well as the development of thrombocytopenia;
• manifestations of allergies: rashes and itching, as well as hives. There is an allergic rhinitis;
• other: the development of impotence, gynecomastia or alopecia, and in addition, a disorder of the menstrual cycle and the emergence of paresthesias.

As a result of local use of the cream, itching and burning with irritation at the treatment site were observed. In the case of using shampoo, hair color can change or fall out.

If the patient has any negative reactions, you need to cancel the medicine and consult the doctor.

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Overdose

Intoxication with topical use.

In case of application of the cream in excessive amounts, the skin may appear with puffiness or erythema, as well as a sensation of a skin burn. These symptoms quickly disappear after withdrawal of drugs.

When using tablets, an overdose manifests as a vomiting with nausea, as well as dizziness with a headache. With further increase in dosage, tingling and spasms may occur.

The medicine does not have an antidote. To eliminate the disorders, it is necessary to cancel the medicine, rinse the stomach and give the affected enterosorbents. Symptomatic treatment is also used.

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Interactions with other drugs

Interaction of tablets.

Drugs that reduce the pH level in the stomach, reduce the degree of absorption of ketoconazole. Therefore, in the case of combined use of these drugs, it is required to keep the intervals between receptions - at least 2 hours.

Rifampicin with isoniazid in combination with Dermazol reduces the latter's indices inside the plasma.

Due to the blockade of liver enzymes under the action of ketoconazole in the hemoprotein P450 system, the period of drug effect of drugs that are directly metabolized by these enzymes is increased. Since inhibition of metabolic processes is carried out, the probability of negative effects of these drugs increases.

Among the potentially dangerous combinations: statins, astemizole, terfenadine with midazolam, and in addition cisapride with triazolam for internal administration. Ketoconazole increases the values of these drugs inside the plasma, which can cause negative reactions from the CCC. Therefore, it is forbidden to take these medicines together. 

Ketoconazole prolongs the period of sedation effected by intravenous infusion of midazolam.

When combined with Dermazol, dosage adjustments of cyclosporine with bisulfane, as well as anticoagulants with methylprednisolone, should be adjusted.

Ketoconazole can not be combined with ethyl alcohol (a combination of these drugs leads to the development of a disulfiram-like effect), which requires that you stop drinking alcohol during treatment with Dermazol.

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Storage conditions

The medicine should be kept in a dark place inaccessible to small children. Temperature conditions - maximum 25 ° C.

Shelf life

Dermazol is allowed to be used in the period of 3 years from the date of release of the medicine.